Topoisomerase
Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.
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Topoisomerase Inhibitors
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Topoisomerase Agonists
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Topoisomerase Modulator
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Topoisomerase Inducer
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Topoisomerase Degraders
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Topoisomerase Controls
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Topoisomerase Ligands
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Topoisomerase Proteins
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DNA topoisomerase II Proteins
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Topoisomerase Verwandte Produkte (838)
Verwandte Produkte (838)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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ADC Control Human IgG1-JSSW-001
0 ImagesArt. -Nr.: HY-185833ADC Control Human IgG1-JSSW-001 is the isotype control for ADC SYS6010 (HY-185832). SYS6010 is an antibody-drug conjugate (ADC) targeting epidermal growth factor receptor (EGFR), which is formed by conjugating the anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) with the topoisomerase I inhibitor JS-1 (HY-178217) via a cleavable tetrapeptide linker. SYS6010 can be used in the research of advanced solid tumors such as non-small cell lung cancer.
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GENA-104A16
0 ImagesArt. -Nr.: HY-P992356GENA-104A16 is a humanized monoclonal antibody targeting CNTN4, with multiple functions including immunostimulation, cytotoxicity and immunoregulation. By binding to CNTN4, GENA-104A16 blocks its interaction with APP, thereby restoring T cell function, inducing tumor cell death and regulating tumor-infiltrating immune cell populations. GENA-104A16 also exerts topoisomerase I inhibitory activity via the payload Exatecan (HY-13631). GENA-104A16 can be used in research related to colon cancer liver metastasis and other CNTN4-expressing solid tumors.
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Topoisomerase I/II-IN-9
0 ImagesArt. -Nr.: HY-182926Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer.
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Topotecan acetate
0 ImagesArt. -Nr.: HY-13768DCAS. Nr.: 123948-88-9Synonyms: SKF 104864A acetate; NSC 609669 acetateTopotecan acetate is a topoisomerase inhibitor.
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Topoisomerase IIα-IN-6
0 ImagesArt. -Nr.: HY-152473CAS. Nr.: 3042869-61-1Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism.
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Topoisomerase I inhibitor 5
0 ImagesArt. -Nr.: HY-144774CAS. Nr.: 2513461-95-3Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
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TOP1 Human Pre-designed siRNA Set A
0 ImagesArt. -Nr.: HY-RS14890TOP1 Human Pre-designed siRNA Set A contains three designed siRNAs for TOP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Topoisomerase IIα-IN-2
0 ImagesArt. -Nr.: HY-146021CAS. Nr.: 2407521-90-6Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase.
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Topoisomerase IIα-IN-4
0 ImagesArt. -Nr.: HY-151453CAS. Nr.: 2860554-26-1Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.
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Topoisomerase IN-7
0 ImagesArt. -Nr.: HY-189061Topoisomerase IN-7 is a bacterial topoisomerase inhibitor, with an IC50 value of 47 nM against Staphylococcus aureus DNA gyrase, 85 nM against Escherichia coli DNA gyrase, and 1 nM against Escherichia coli topoisomerase IV. Topoisomerase IN-7 inhibits the supercoiling activity of DNA gyrase, suppresses the relaxation activity of topoisomerase IV, stabilizes single-stranded DNA cleavage complexes, inhibits biofilm formation of specific bacteria, stimulates biofilm formation of methicillin-resistant Staphylococcus aureus, and exhibits bactericidal activity. Topoisomerase IN-7 is selective for bacterial topoisomerases over human topoisomerase IIα, shows moderate cytotoxicity, and inhibits the hERG potassium channel. Topoisomerase IN-7 can be used in studies of bacterial infections.
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Val-Cit-Exatecan
0 ImagesArt. -Nr.: HY-160756CAS. Nr.: 2952679-21-7Val-Cit-Exatecan is a peptide-linked anti-tumor payload that can be used for the synthesis of antibody-drug conjugates (ADC). Val-Cit-Exatecan consists of DNA TopI inhibitor Exatecan (HY-13631) and a cathepsin-cleavable ADC linker (valine-citrulline). Val-Cit-Exatecan can be used in the research of colorectal cancer, gastric cancer, breast cancer, non-small cell lung cancer, ovarian cancer, head and neck cancer, pancreatic cancer, cervical cancer, and melanoma.
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Topoisomerase II inhibitor 23
0 ImagesArt. -Nr.: HY-174404Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
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NISC-6
0 ImagesArt. -Nr.: HY-153685CAS. Nr.: 2097636-49-0
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GC-072
0 ImagesArt. -Nr.: HY-178738CAS. Nr.: 1371629-36-5GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis.
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Fagopyrine
0 ImagesArt. -Nr.: HY-162587CAS. Nr.: 72393-03-4Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors.
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Topoisomerase II/EGFR-IN-2
0 ImagesArt. -Nr.: HY-180823Topoisomerase II/EGFR-IN-2 (Compound 3) is an inhibitor of Topoisomerase IIα (IC50 = 0.122 μM) and EGFR-TKWT (IC50 = 16.8 μM). Topoisomerase II/EGFR-IN-2 inhibits the proliferation of HeLa and HepG2 cells, inducing cell cycle arrest and apoptosis. Topoisomerase II/EGFR-IN-2 upregulates caspase-3 and Bax, and downregulates Bcl-2. Topoisomerase II/EGFR-IN-2 can be used to study liver cancer and cervical cancer.
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SeSA-HCPT
0 ImagesArt. -Nr.: HY-181694SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity.
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Topoisomerase I inhibitor 14
0 ImagesArt. -Nr.: HY-162342CAS. Nr.: 3033693-30-7Topoisomerase I inhibitor 14 (Compound 4h) is an inhibitor for Topoisomerase I. Topoisomerase I inhibitor 14 inhibits proliferation of A549 and C6 with IC50s of 4.56 μM and 13.17 μM, without significant toxicity in healthy cells NIH3T3 (IC50 is 74.44 μM), which exhibits anticancer potency.
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3-Fluoro-evodiamine glucose
0 ImagesArt. -Nr.: HY-161501Reinheit: 99.95%3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity.
